195137-95-2

Usage

Uses

Used in Pharmaceutical Research and Drug Development:
(S)-5-[(Biphenyl-4-yl)carbonyl]pyrrolidin-2-one is used as a building block for the synthesis of biologically active compounds, contributing to the development of new pharmaceutical agents.
Used in Therapeutic Applications:
(S)-5-[(Biphenyl-4-yl)carbonyl]pyrrolidin-2-one is used as a potential drug candidate for various therapeutic applications, owing to its pharmacological properties and ability to interact with specific biological targets.
Used in Medicinal Chemistry:
In the field of medicinal chemistry, (S)-5-[(Biphenyl-4-yl)carbonyl]pyrrolidin-2-one is employed as a key component in the design and synthesis of novel drug molecules, targeting a variety of diseases and conditions.

Upstream product

• 85187-29-7 (S)-5-(morpholine-4-carbonyl)pyrrolidin-2-one 
• 92-52-4 biphenyl 
• 74936-93-9 (S)-5-oxopyrrolidine-2-carbonyl chloride 
• 92-66-0 4-bromo-1,1'-biphenyl 
• 77-92-9 citric acid 
• 3315-91-1 4-biphenylylmagnesium bromide 
• 51959-85-4 (R/S)-5-(morpholine-4-carbonyl)pyrrolidin-2-one 
• 7439-95-4 magnesium 

Downstream Products

• 1038924-77-4 (S)-2-biphenyl-4-ylmethyl-5-oxopyrrolidine-1-carboxylic acid tert-butyl ester 
• 1038924-61-6 (S)-5-biphenyl-4-ylmethylpyrrolidin-2-one 

Relevant academic research and scientific papers

A Entresto intermediate (S)- 5 - (biphenyl - 4 - carbonyl) pyrrolidine - 2 - one synthetic method

The invention discloses a synthetic method of Entresto midbody (S)-5-(diphenyl-4-carbonyl) pyrrolidine-2-ketone. The synthetic method comprises the following steps: taking (S)-5-(morpholine-4-carbonyl) pyrrolidine-2-ketone and (chloromethyl) benzene as raw materials, dissolving in organic solvent, and obtaining (S)-1-benzyl-5-(morpholine-4-carbonyl) pyrrolidine-2-ketone under the action of alkali, then reacting with an organic solution of 4-diphenyl magnesium bromide, and carrying out the debenzylation reaction to generate the Entresto midbody (S)-5-(diphenyl-4-carbonyl) pyrrolidine-2-ketone. By adopting the synthetic method, the dosage of diphenyl magnesium bromide is remarkably reduced, so that the production cost is obviously reduced, and the production period is greatly shortened; during the process for manufacturing a diphenyl magnesium bromide Grignard reagent, the yield is relatively low. According to the synthetic method, due to the reduction of the dosage of the diphenyl magnesium bromide, the danger coefficient is also reduced (the production is safer). The synthetic method is more suitable for the industrialized production.

A method for the synthesis of pharmaceutical intermediates

The invention relates to the field of medical chemistry, in particular relates to the field of pharmaceutical synthesis, and more particularly relates to a synthesis method for a medical intermediate. The synthesis method comprises the following steps: firstly enabling a compound I to react with oxalyl chloride to prepare a compound II; and directly adding a reaction liquid to a compound III through treatment or absence of treatment, so as to obtain a compound IV. The synthesis route provided by the invention is simple in production technology, high in product yield, and simple in purification and treatment; and the product is high in purity after being simply treated, low in preparation cost and suitable for industrialized production.

THERAPEUTIC AGENT FOR DIABETES

A therapeutic agent for diabetes, which comprises a compound of the formula [I] wherein Xis a group of the formula wherein R4and R5are the same or different and each is a hydrogen atom, an optionally substituted alkyl having 1 to 5 carbon atoms and the like, and R6is a hydrogen atom or an amino-protecting group; R1is an optionally substituted alkyl having 1 to 5 carbon atoms, an optionally substituted alkenyl having 2 to 6 carbon atoms and the like, R2is a hydrogen atom, an optionally substituted alkyl having 1 to 5 carbon atoms and the like, R2' is a hydrogen atom, and R3is an optionally substituted alkyl having 1 to 5 carbon atoms and the like, a prodrug thereof, a pharmaceutically acceptable salt thereof, a hydrate thereof and a solvate thereof. The compound of the present invention shows superior blood sugar decreasing action on the state of hyperglycemia, but does not affect the blood sugar when it is in the normal range or in the hypoglycemic state, which means that it is free of serious side effects such as hypoglycemia. Therefore, the compound of the present invention is useful as a therapeutic drug for diabetes and also useful as a preventive of the chronic complications of diabetes.